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68 Cards in this Set
- Front
- Back
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diuretics
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thiazides (hydrochlorothiazide)
loop diuretics (furosemide) k sparing diuretics (spironolactone) |
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Inhibitors of the RAA system
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ACE inhibitors (lisinopril)
angiotensin receptor blockers (losartan) |
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Vasodilators
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direct acting (nitroprusside and hydralazine)
calcium entry blockers (verapamil, nifedipine) |
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Sympatholytic agents
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act within CNS (clonidine)
act on autonomic ganglia (trimethaphan) act on post-ganglionic neurons (reserpine) block peripheral adrenergic receptors (atenolol, prazosin, labetolol) |
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Drug class of hydrocholorothiazide
(HydroDiuril) |
pharmacologic class - thiazide diuretic
therapeutic class - diuretic, antihypertensive |
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Pharmacodynamics of hydrochlorothiazide
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blocks the reuptake of Cl and Na from tubular fluid after glomerular filtration; also appears to cause decrease in SVR, unclear mechanism; will lower BP by up to 10-15mm in may patients; is useful as a monotherapy or in combinations
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Pharmacokinetics of hydrochlorothiazide
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F - 70%, excreted unchanged in urine; short half-life (hours); HCTZ not available in IV formulation; onset 2 hours, peak 5 hours, duration 10 hours
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Toxicity of hydrochlorothiazide
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allergy to sulfa antibiotics; cause K and Mg depletion; cause Na and Cl depletion, metabolic alkalosis; volume depletion; worsen hyperuricemia
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Interactions of hydrochlorothiazide
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additive effects with most other antihypertensives
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Special considerations for hydrochlorothiazide
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more side effects in geriatric patients; pregnancy class D; ineffective in patients with significant renal disease
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Indications and dose/route with hydrochlorothiazide
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12.5 mg or 25 mg po every morning; little benefit (more toxicity) when given in higher doses
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Monitoring of hydrochlorothiazide
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BP, weight, edema, K, Mg, BUN, creatinine
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Lisinopril
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(Prinivil; also captopril, enalapril, ramipril)
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Drug class of lisinopril
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pharmacologic class - ACE inhibitor; therapeutic antihypertensive, treatment of CHF, preserving renal function, preserving LV function after MI, acute management of MI
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Pharmacodynamics of Lisinopril
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inhibits the conversion of AT I to AT II by ACE; diminishes both vasocontriction and stimulation of aldosterone secretion by AT II
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Pharmacokinetics of Lisinopril
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well absorbed; onset 1 hour, peak 6 hours, duration 24 hours; once a day is fine; excreted primarily in urine as unchanged drug
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Toxicity of lisinopril
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orthostatic hypotension; use with caution in patients with impaired renal function, or renal artery stenosis; be careful in patients on diuretics, or those with aortic stenosis; angioedema; acute renal failure
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Interactions of lisinopril
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additive effects with most other antihypertensives; NSAIDS may reduce ability to lower BP; hyperkalemia with KCL, others;
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Special considerations of lisinopril
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often discontinue diuretics prior to beginning use to reduce hypotension; category C/D in pregnancy, abnormal cartilage development
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Indications and dose/route of lisinopril
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begin 10mg per day, titrate slowly upward to 40 mg per day max
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Monitoring of lisinopril
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BP, weight, edema, K, BUN, creatinine, cough
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Losartan
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(CoZaar, also irbesartan, etc)
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Drug Class of Losartan
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pharmacologic class: angiotensin I receptor blocker (ARB)
therapeutic class: diuretic, antihypertensive, preserve renal function, treatment of CHF |
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Pharmacodynamics of Losartan
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block stimulation of AT I receptor by angiotensin II, thereby reducing vasoconstriction and productiong of aldosterone
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Pharmacokinetics of Losartan
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F ~ 30%; onset 6 hours; extensive first pass effect; active metabolite is 40x more potent, much longer half-life
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Toxicity of Losartan
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dizziness; orthostatic hypotension; worsening of renal failure
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Interactions of Losartan
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additive effects with most other antihypertensives
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Special considerations of Losartan
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pregnancy class C/D; use care in patients on diuretics, those with renal artery stenosis, those with mitral or aortic stenosis
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Indications and dose/route
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1 for hypertension, daily doses 25-100mg every day
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Special considerations for hydrochlorothiazide
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more side effects in geriatric patients; pregnancy class D; ineffective in patients with significant renal disease
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Indications and dose/route with hydrochlorothiazide
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12.5 mg or 25 mg po every morning; little benefit (more toxicity) when given in higher doses
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Monitoring of hydrochlorothiazide
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BP, weight, edema, K, Mg, BUN, creatinine
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Lisinopril
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(Prinivil; also captopril, enalapril, ramipril)
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Drug class of lisinopril
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pharmacologic class - ACE inhibitor; therapeutic antihypertensive, treatment of CHF, preserving renal function, preserving LV function after MI, acute management of MI
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Pharmacodynamics of Losartan
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block stimulation of AT I receptor by angiotensin II, thereby reducing vasoconstriction and production of aldosterone
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Pharmacokinetics of Losartan
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F ~ 30%; onset 6 hours; extensive first pass effect; active metabolite in 40x more potent, much longer half-life
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Toxicity of Losartan
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dizziness, orthostatic hypotension; worsening of renal failure
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Interactions of Losartan
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additive effects with most other antihypertensives
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Special considerations of Losartan
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pregnancy class C/D; use care in patients on diuretics, those with renal artery stenosis; those with mitral or aortic stenosis
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Indications and dose/route of Losartan
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1 for HTN, daily doses 25-100mg every day
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Monitoring of Losartan
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BP, weight, edema, electrolytes, BUN, and creatinine
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Nitroprusside
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Nipride, Nitropress
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Drug class of nitroprusside
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pharmacologic vasodilator
therapeutic class: antihypertensive, management of CHF, management of pulmonary hypertension, produce controlled hypotension to reduce bleeding during surgery |
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Pharmacodynamics of nitroprusside
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acts "directly" on vascular smooth muscle to cause dilatation of both veins and arterioles; metabolized to release CN- and NO, which activates guanylate cyclase, leads to production of cGMP from GTP, which then leads to vasodilation; cGMP then hydrolzed to GMP by PDE
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Pharmacokinetics of nitroprusside
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only route is via iv; rapid onset (minutes) and cessation (minutes), thereby allowing minute-by-minute titration; CN- metabolite is converted to SCN in the liver, then excreted in the urine; must be given by continuous infusion
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Toxicity of nitroprusside
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excessive hypotension; accumulation of CN and thiocyanate; headache; decreased blood flow to brain
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Interactions of nitroprusside
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additive effects with most other antihypertensives
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Special considerations of nitroprusside
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monitor very closely; avoid high infusion rates or prolonged infusions, to prevent accumulation of CN-; use with caution in patients with increase intracranial pressure
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Indications and dose/route of nitroprusside
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for treatment of hypertensive crisis, given as IV infusion at 0.3-10 mcg/kg per minute; do not exceed 24 hours of infusion
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Monitoring of nitroprusside
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BP, HR, metabolic acidosis; most often requires an arterial line
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Hydralazine
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apresoline
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Drug class of hydralazine
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pharmacologic class: peripheral vasodilator
therapeutic class: antihypertensive, treatment of CHF, vasodilator |
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Pharmacodynamics of hydralazine
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"direct" acting vasodilator; may act by inducing endothelium to produce NO, which then passes to SM cells and induces production of cGMP, minimal venodilating effect
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Pharmacokinetics of hydralazine
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given po, im, iv; metabolized extensively in GI mucosa and in the liver; eventually excreted as metabolites in urine; F ~ 40%; onset 30 after po dose, 10 minutes after iv dose; persist for 2-6 hours
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Toxicity of hydralazine
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more dangerous in patients with renal disease, prior to stroke, angina; watch for hypotension, edema, occasionally drug induced lupus
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Interactions of hydralazine
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additive effects with most other antihypertensives
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Special considerations of hydralazine
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never use as a monotherapy for treatment of hypertension, since edema and reflex tachcardia will result, concert giving to patients with CAD
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Indications and dose/route of hydralazine
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dose 10-50mg po four times daily
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Monitoring hydralazine
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BP, weight, edema, BUN, creatinine, symptoms of lupus or angina
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Verapamil
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Isoptin, Calan, similar to nifedipine, amlodipine, diltiazem, etc
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Drug class of verapamil
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pharmacologic class: calcium entry blocker
therapeutic class: antihypertensive, antianginal, and antiarrhythmic |
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Pharmacodynamics of verapamil
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reduces BP by inhibiting influx of calcium through "slow channels", thereby dilating peripheral arterioles; produces negative inotropic effect as well; for angina, reduces afterload, thus decreasing oxygen consumption; also, inhibits spasm of coronary arteries in vasospastic angina; blocks re-entry paths through AV node in paroxysmal SVT
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Pharmacokinetics of verapamil
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absorbed rapidly, but F ~ 30%
also available in SR tablets; cleared by kidney and liver (produces active metabolites); onset 2 hours po, 1-5 min iv; half-life 6-12 hours; may be given po or iv |
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Toxicity of verapamil
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hypotension, AV block, worsening of CHF, bradycardia
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Interactions of verapamil
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additive effects with most other antihypertensives; additive toxic effects on heart when given with beta-blockers
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Special considerations of verapamil
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use reduced doses in patients with both renal and hepatic disease; short-acting nifedipine (and similar CEBs) can increase risk of MI (unclear why); Pregnancy C
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Indications and dose/route for verapamil
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80mg thrice daily, or 240 mg SR once daily
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Monitoring of verapamil
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hypotension, orthostasis, worsening CHF or conduction
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